ES2163384T3 - Receptores acoplados a proteinas g humanos, activados de forma constitutiva, no endogenos. - Google Patents
Receptores acoplados a proteinas g humanos, activados de forma constitutiva, no endogenos.Info
- Publication number
- ES2163384T3 ES2163384T3 ES99951991T ES99951991T ES2163384T3 ES 2163384 T3 ES2163384 T3 ES 2163384T3 ES 99951991 T ES99951991 T ES 99951991T ES 99951991 T ES99951991 T ES 99951991T ES 2163384 T3 ES2163384 T3 ES 2163384T3
- Authority
- ES
- Spain
- Prior art keywords
- endogenous
- baselineskip
- sec
- gpcr
- human
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 102000003839 Human Proteins Human genes 0.000 title 1
- 108090000144 Human Proteins Proteins 0.000 title 1
- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 claims abstract description 169
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 claims abstract description 169
- 102000005962 receptors Human genes 0.000 claims abstract description 138
- 108020003175 receptors Proteins 0.000 claims abstract description 138
- 241000282414 Homo sapiens Species 0.000 claims abstract description 112
- 150000001875 compounds Chemical class 0.000 claims abstract description 76
- 108020004705 Codon Proteins 0.000 claims abstract description 34
- 230000003834 intracellular effect Effects 0.000 claims abstract description 28
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims abstract description 27
- 239000004472 Lysine Substances 0.000 claims abstract description 26
- 125000000539 amino acid group Chemical group 0.000 claims abstract description 23
- 101000887490 Homo sapiens Guanine nucleotide-binding protein G(z) subunit alpha Proteins 0.000 claims abstract description 8
- 102000052301 human GNAZ Human genes 0.000 claims abstract description 8
- 238000000034 method Methods 0.000 claims description 61
- 239000000556 agonist Substances 0.000 claims description 33
- 125000001500 prolyl group Chemical group [H]N1C([H])(C(=O)[*])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 21
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 11
- 239000004031 partial agonist Substances 0.000 claims description 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 10
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims description 8
- 235000004279 alanine Nutrition 0.000 claims description 8
- 239000004475 Arginine Substances 0.000 claims description 7
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims description 7
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims description 7
- 229940125425 inverse agonist Drugs 0.000 claims description 6
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 230000002441 reversible effect Effects 0.000 claims description 3
- 125000000430 tryptophan group Chemical group [H]N([H])C(C(=O)O*)C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12 0.000 claims description 3
- 230000036961 partial effect Effects 0.000 claims description 2
- 108091033319 polynucleotide Proteins 0.000 claims 5
- 102000040430 polynucleotide Human genes 0.000 claims 5
- 239000002157 polynucleotide Substances 0.000 claims 5
- 150000007523 nucleic acids Chemical group 0.000 abstract description 133
- 102000039446 nucleic acids Human genes 0.000 abstract description 98
- 108020004707 nucleic acids Proteins 0.000 abstract description 98
- 230000035772 mutation Effects 0.000 abstract description 35
- 239000012528 membrane Substances 0.000 abstract description 18
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 abstract description 17
- 125000003275 alpha amino acid group Chemical group 0.000 abstract description 15
- 210000004962 mammalian cell Anatomy 0.000 abstract description 13
- 230000001413 cellular effect Effects 0.000 abstract description 5
- 108091028043 Nucleic acid sequence Proteins 0.000 abstract description 3
- 238000012216 screening Methods 0.000 abstract 1
- 235000001014 amino acid Nutrition 0.000 description 159
- 229940024606 amino acid Drugs 0.000 description 159
- 150000001413 amino acids Chemical class 0.000 description 155
- 108020004414 DNA Proteins 0.000 description 109
- 239000002299 complementary DNA Substances 0.000 description 72
- 210000004027 cell Anatomy 0.000 description 65
- 108090000623 proteins and genes Proteins 0.000 description 63
- 239000012634 fragment Substances 0.000 description 56
- 239000013604 expression vector Substances 0.000 description 55
- 238000004458 analytical method Methods 0.000 description 48
- 101000829902 Homo sapiens G-protein coupled estrogen receptor 1 Proteins 0.000 description 47
- 102100023328 G-protein coupled estrogen receptor 1 Human genes 0.000 description 45
- 102000004169 proteins and genes Human genes 0.000 description 43
- 235000018102 proteins Nutrition 0.000 description 42
- 230000014509 gene expression Effects 0.000 description 41
- 239000013598 vector Substances 0.000 description 38
- 239000002773 nucleotide Substances 0.000 description 34
- 125000003729 nucleotide group Chemical group 0.000 description 34
- 239000007853 buffer solution Substances 0.000 description 30
- XOFLBQFBSOEHOG-UUOKFMHZSA-N γS-GTP Chemical compound C1=2NC(N)=NC(=O)C=2N=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=S)[C@@H](O)[C@H]1O XOFLBQFBSOEHOG-UUOKFMHZSA-N 0.000 description 25
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 24
- 239000013612 plasmid Substances 0.000 description 23
- 239000006274 endogenous ligand Substances 0.000 description 22
- 239000003446 ligand Substances 0.000 description 22
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 description 21
- 230000004913 activation Effects 0.000 description 21
- 210000001519 tissue Anatomy 0.000 description 21
- 102100033861 G-protein coupled receptor 6 Human genes 0.000 description 19
- 101001069613 Homo sapiens G-protein coupled receptor 6 Proteins 0.000 description 19
- 108091006027 G proteins Proteins 0.000 description 17
- 102000030782 GTP binding Human genes 0.000 description 17
- 108091000058 GTP-Binding Proteins 0.000 description 17
- 230000004044 response Effects 0.000 description 16
- 101000793362 Homo sapiens Apelin receptor Proteins 0.000 description 15
- 210000004556 brain Anatomy 0.000 description 15
- 239000003550 marker Substances 0.000 description 15
- 102100030949 Apelin receptor Human genes 0.000 description 14
- 108060001084 Luciferase Proteins 0.000 description 14
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 description 13
- 238000001890 transfection Methods 0.000 description 13
- 239000006144 Dulbecco’s modified Eagle's medium Substances 0.000 description 12
- 239000005089 Luciferase Substances 0.000 description 12
- 108091000080 Phosphotransferase Proteins 0.000 description 12
- 239000000872 buffer Substances 0.000 description 12
- 230000000694 effects Effects 0.000 description 12
- 239000000203 mixture Substances 0.000 description 12
- 102000020233 phosphotransferase Human genes 0.000 description 12
- 229940076279 serotonin Drugs 0.000 description 12
- 230000001225 therapeutic effect Effects 0.000 description 12
- 101000829770 Homo sapiens Uracil nucleotide/cysteinyl leukotriene receptor Proteins 0.000 description 11
- 230000006552 constitutive activation Effects 0.000 description 11
- 230000007423 decrease Effects 0.000 description 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 11
- 101000750094 Homo sapiens Chemerin-like receptor 2 Proteins 0.000 description 10
- 230000008859 change Effects 0.000 description 10
- 239000002609 medium Substances 0.000 description 10
- 102100021198 Chemerin-like receptor 2 Human genes 0.000 description 9
- 102000005636 Cyclic AMP Response Element-Binding Protein Human genes 0.000 description 9
- 108010045171 Cyclic AMP Response Element-Binding Protein Proteins 0.000 description 9
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 9
- 241000124008 Mammalia Species 0.000 description 9
- 102100023407 Uracil nucleotide/cysteinyl leukotriene receptor Human genes 0.000 description 9
- 239000003814 drug Substances 0.000 description 9
- 239000000523 sample Substances 0.000 description 9
- 210000000952 spleen Anatomy 0.000 description 9
- 239000000126 substance Substances 0.000 description 9
- 101000871138 Homo sapiens G-protein coupled receptor 4 Proteins 0.000 description 8
- TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 description 8
- 239000005557 antagonist Substances 0.000 description 8
- 201000010099 disease Diseases 0.000 description 8
- 102100033045 G-protein coupled receptor 4 Human genes 0.000 description 7
- 239000002253 acid Substances 0.000 description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 7
- UQLLWWBDSUHNEB-CZUORRHYSA-N Cefaprin Chemical compound N([C@H]1[C@@H]2N(C1=O)C(=C(CS2)COC(=O)C)C(O)=O)C(=O)CSC1=CC=NC=C1 UQLLWWBDSUHNEB-CZUORRHYSA-N 0.000 description 6
- 102100035294 Chemokine XC receptor 1 Human genes 0.000 description 6
- 102100023416 G-protein coupled receptor 15 Human genes 0.000 description 6
- 101001071349 Homo sapiens 12-(S)-hydroxy-5,8,10,14-eicosatetraenoic acid receptor Proteins 0.000 description 6
- 101000922405 Homo sapiens C-X-C chemokine receptor type 5 Proteins 0.000 description 6
- 101000804783 Homo sapiens Chemokine XC receptor 1 Proteins 0.000 description 6
- 101000829794 Homo sapiens G-protein coupled receptor 15 Proteins 0.000 description 6
- 101001071355 Homo sapiens G-protein coupled receptor 20 Proteins 0.000 description 6
- 101001071360 Homo sapiens G-protein coupled receptor 22 Proteins 0.000 description 6
- 101001035752 Homo sapiens Hydroxycarboxylic acid receptor 3 Proteins 0.000 description 6
- 101000829761 Homo sapiens N-arachidonyl glycine receptor Proteins 0.000 description 6
- 101000603407 Homo sapiens Neuropeptides B/W receptor type 1 Proteins 0.000 description 6
- 101000603411 Homo sapiens Neuropeptides B/W receptor type 2 Proteins 0.000 description 6
- 101000829779 Homo sapiens Probable G-protein coupled receptor 19 Proteins 0.000 description 6
- 101001071363 Homo sapiens Probable G-protein coupled receptor 21 Proteins 0.000 description 6
- 101001009517 Homo sapiens Probable G-protein coupled receptor 32 Proteins 0.000 description 6
- 101001123492 Homo sapiens Prolactin-releasing peptide receptor Proteins 0.000 description 6
- 101001026578 Hordeum vulgare Ent-kaurenoic acid oxidase 1 Proteins 0.000 description 6
- 102100029002 Prolactin-releasing peptide receptor Human genes 0.000 description 6
- 102000001708 Protein Isoforms Human genes 0.000 description 6
- 108010029485 Protein Isoforms Proteins 0.000 description 6
- 101710120037 Toxin CcdB Proteins 0.000 description 6
- 238000001514 detection method Methods 0.000 description 6
- 229940079593 drug Drugs 0.000 description 6
- 238000007876 drug discovery Methods 0.000 description 6
- 229960000367 inositol Drugs 0.000 description 6
- 241000894007 species Species 0.000 description 6
- 238000012546 transfer Methods 0.000 description 6
- JKMHFZQWWAIEOD-UHFFFAOYSA-N 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid Chemical compound OCC[NH+]1CCN(CCS([O-])(=O)=O)CC1 JKMHFZQWWAIEOD-UHFFFAOYSA-N 0.000 description 5
- 102100028990 C-X-C chemokine receptor type 3 Human genes 0.000 description 5
- 101710085500 C-X-C motif chemokine 9 Proteins 0.000 description 5
- 102100033047 G-protein coupled receptor 3 Human genes 0.000 description 5
- 108010016122 Ghrelin Receptors Proteins 0.000 description 5
- 102100039256 Growth hormone secretagogue receptor type 1 Human genes 0.000 description 5
- 239000007995 HEPES buffer Substances 0.000 description 5
- 101000916050 Homo sapiens C-X-C chemokine receptor type 3 Proteins 0.000 description 5
- 101000912510 Homo sapiens Free fatty acid receptor 1 Proteins 0.000 description 5
- 101000890668 Homo sapiens Free fatty acid receptor 2 Proteins 0.000 description 5
- 101000890662 Homo sapiens Free fatty acid receptor 3 Proteins 0.000 description 5
- 101000871088 Homo sapiens G-protein coupled receptor 3 Proteins 0.000 description 5
- 101001063456 Homo sapiens Leucine-rich repeat-containing G-protein coupled receptor 5 Proteins 0.000 description 5
- 101000581402 Homo sapiens Melanin-concentrating hormone receptor 1 Proteins 0.000 description 5
- 101001120710 Homo sapiens Ovarian cancer G-protein coupled receptor 1 Proteins 0.000 description 5
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 description 5
- 102100031036 Leucine-rich repeat-containing G-protein coupled receptor 5 Human genes 0.000 description 5
- 102100038847 Neuropeptides B/W receptor type 1 Human genes 0.000 description 5
- 238000009825 accumulation Methods 0.000 description 5
- 108010005774 beta-Galactosidase Proteins 0.000 description 5
- 210000000170 cell membrane Anatomy 0.000 description 5
- 238000006243 chemical reaction Methods 0.000 description 5
- 230000001605 fetal effect Effects 0.000 description 5
- 238000011534 incubation Methods 0.000 description 5
- 230000005764 inhibitory process Effects 0.000 description 5
- 230000001404 mediated effect Effects 0.000 description 5
- 210000002826 placenta Anatomy 0.000 description 5
- 239000002244 precipitate Substances 0.000 description 5
- 239000013049 sediment Substances 0.000 description 5
- 210000002966 serum Anatomy 0.000 description 5
- 239000000243 solution Substances 0.000 description 5
- 102100036933 12-(S)-hydroxy-5,8,10,14-eicosatetraenoic acid receptor Human genes 0.000 description 4
- 101710149858 C-C chemokine receptor type 7 Proteins 0.000 description 4
- 102100036301 C-C chemokine receptor type 7 Human genes 0.000 description 4
- 102100031658 C-X-C chemokine receptor type 5 Human genes 0.000 description 4
- 102100040133 Free fatty acid receptor 2 Human genes 0.000 description 4
- 102100040136 Free fatty acid receptor 3 Human genes 0.000 description 4
- 101710101406 G-protein coupled receptor 183 Proteins 0.000 description 4
- 102100021245 G-protein coupled receptor 183 Human genes 0.000 description 4
- 102100036939 G-protein coupled receptor 20 Human genes 0.000 description 4
- 102100036940 G-protein coupled receptor 22 Human genes 0.000 description 4
- 101100323464 Homo sapiens APLNR gene Proteins 0.000 description 4
- 102100039356 Hydroxycarboxylic acid receptor 3 Human genes 0.000 description 4
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 description 4
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 description 4
- 102100027375 Melanin-concentrating hormone receptor 1 Human genes 0.000 description 4
- 102100023414 N-arachidonyl glycine receptor Human genes 0.000 description 4
- 102100038843 Neuropeptides B/W receptor type 2 Human genes 0.000 description 4
- 102000016978 Orphan receptors Human genes 0.000 description 4
- 108070000031 Orphan receptors Proteins 0.000 description 4
- 102100023417 Probable G-protein coupled receptor 19 Human genes 0.000 description 4
- 102100036934 Probable G-protein coupled receptor 21 Human genes 0.000 description 4
- 102100030321 Probable G-protein coupled receptor 32 Human genes 0.000 description 4
- 108091027981 Response element Proteins 0.000 description 4
- 102000030621 adenylate cyclase Human genes 0.000 description 4
- 108060000200 adenylate cyclase Proteins 0.000 description 4
- 102000005936 beta-Galactosidase Human genes 0.000 description 4
- 238000012761 co-transfection Methods 0.000 description 4
- 230000008878 coupling Effects 0.000 description 4
- 238000010168 coupling process Methods 0.000 description 4
- 238000005859 coupling reaction Methods 0.000 description 4
- 230000003247 decreasing effect Effects 0.000 description 4
- 238000009826 distribution Methods 0.000 description 4
- 239000013613 expression plasmid Substances 0.000 description 4
- 238000000338 in vitro Methods 0.000 description 4
- 238000001727 in vivo Methods 0.000 description 4
- CDAISMWEOUEBRE-GPIVLXJGSA-N inositol Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]1O CDAISMWEOUEBRE-GPIVLXJGSA-N 0.000 description 4
- 210000004072 lung Anatomy 0.000 description 4
- 229910001629 magnesium chloride Inorganic materials 0.000 description 4
- 238000005259 measurement Methods 0.000 description 4
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 description 4
- 230000004048 modification Effects 0.000 description 4
- 238000012986 modification Methods 0.000 description 4
- 230000001817 pituitary effect Effects 0.000 description 4
- 102000054765 polymorphisms of proteins Human genes 0.000 description 4
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 description 4
- 210000001541 thymus gland Anatomy 0.000 description 4
- 108091032973 (ribonucleotides)n+m Proteins 0.000 description 3
- 102000002260 Alkaline Phosphatase Human genes 0.000 description 3
- 108020004774 Alkaline Phosphatase Proteins 0.000 description 3
- 108091026890 Coding region Proteins 0.000 description 3
- 102100026148 Free fatty acid receptor 1 Human genes 0.000 description 3
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 3
- SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 description 3
- 241000282412 Homo Species 0.000 description 3
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 description 3
- 108091026898 Leader sequence (mRNA) Proteins 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 108091034117 Oligonucleotide Proteins 0.000 description 3
- 102100026070 Ovarian cancer G-protein coupled receptor 1 Human genes 0.000 description 3
- 102000014384 Type C Phospholipases Human genes 0.000 description 3
- 108010079194 Type C Phospholipases Proteins 0.000 description 3
- JLCPHMBAVCMARE-UHFFFAOYSA-N [3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-hydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methyl [5-(6-aminopurin-9-yl)-2-(hydroxymethyl)oxolan-3-yl] hydrogen phosphate Polymers Cc1cn(C2CC(OP(O)(=O)OCC3OC(CC3OP(O)(=O)OCC3OC(CC3O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c3nc(N)[nH]c4=O)C(COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3CO)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cc(C)c(=O)[nH]c3=O)n3cc(C)c(=O)[nH]c3=O)n3ccc(N)nc3=O)n3cc(C)c(=O)[nH]c3=O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)O2)c(=O)[nH]c1=O JLCPHMBAVCMARE-UHFFFAOYSA-N 0.000 description 3
- 238000005119 centrifugation Methods 0.000 description 3
- 238000011161 development Methods 0.000 description 3
- 208000037765 diseases and disorders Diseases 0.000 description 3
- 230000002068 genetic effect Effects 0.000 description 3
- 230000002209 hydrophobic effect Effects 0.000 description 3
- 150000002632 lipids Chemical class 0.000 description 3
- 210000004185 liver Anatomy 0.000 description 3
- -1 lysine amino acid Chemical class 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- 238000002703 mutagenesis Methods 0.000 description 3
- 231100000350 mutagenesis Toxicity 0.000 description 3
- 238000005457 optimization Methods 0.000 description 3
- 108091008880 orphan GPCRs Proteins 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 238000003757 reverse transcription PCR Methods 0.000 description 3
- 238000002741 site-directed mutagenesis Methods 0.000 description 3
- 210000002784 stomach Anatomy 0.000 description 3
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 description 2
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 description 2
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- 108010089448 Cholecystokinin B Receptor Proteins 0.000 description 2
- IVOMOUWHDPKRLL-KQYNXXCUSA-N Cyclic adenosine monophosphate Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-KQYNXXCUSA-N 0.000 description 2
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- BDAGIHXWWSANSR-UHFFFAOYSA-M Formate Chemical compound [O-]C=O BDAGIHXWWSANSR-UHFFFAOYSA-M 0.000 description 2
- 102000013446 GTP Phosphohydrolases Human genes 0.000 description 2
- 108091006109 GTPases Proteins 0.000 description 2
- 108010001515 Galectin 4 Proteins 0.000 description 2
- 102100039556 Galectin-4 Human genes 0.000 description 2
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 2
- 108091006065 Gs proteins Proteins 0.000 description 2
- NYHBQMYGNKIUIF-UUOKFMHZSA-N Guanosine Chemical compound C1=NC=2C(=O)NC(N)=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O NYHBQMYGNKIUIF-UUOKFMHZSA-N 0.000 description 2
- 101000783617 Homo sapiens 5-hydroxytryptamine receptor 2A Proteins 0.000 description 2
- 101000716065 Homo sapiens C-C chemokine receptor type 7 Proteins 0.000 description 2
- 101000947172 Homo sapiens C-X-C motif chemokine 9 Proteins 0.000 description 2
- 101001040801 Homo sapiens G-protein coupled receptor 183 Proteins 0.000 description 2
- 101001066101 Homo sapiens G-protein coupled receptor 37-like 1 Proteins 0.000 description 2
- 101100392414 Homo sapiens GHSR gene Proteins 0.000 description 2
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 description 2
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 2
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 description 2
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 description 2
- 108091036066 Three prime untranslated region Proteins 0.000 description 2
- IQFYYKKMVGJFEH-XLPZGREQSA-N Thymidine Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](O)C1 IQFYYKKMVGJFEH-XLPZGREQSA-N 0.000 description 2
- 102000040945 Transcription factor Human genes 0.000 description 2
- 108091023040 Transcription factor Proteins 0.000 description 2
- IVOMOUWHDPKRLL-UHFFFAOYSA-N UNPD107823 Natural products O1C2COP(O)(=O)OC2C(O)C1N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-UHFFFAOYSA-N 0.000 description 2
- DRTQHJPVMGBUCF-XVFCMESISA-N Uridine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-XVFCMESISA-N 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 description 2
- 230000001919 adrenal effect Effects 0.000 description 2
- 125000003295 alanine group Chemical group N[C@@H](C)C(=O)* 0.000 description 2
- 210000000709 aorta Anatomy 0.000 description 2
- 238000013459 approach Methods 0.000 description 2
- 229910021538 borax Inorganic materials 0.000 description 2
- 239000001506 calcium phosphate Substances 0.000 description 2
- 229910000389 calcium phosphate Inorganic materials 0.000 description 2
- 235000011010 calcium phosphates Nutrition 0.000 description 2
- 238000010367 cloning Methods 0.000 description 2
- 230000000052 comparative effect Effects 0.000 description 2
- 230000037011 constitutive activity Effects 0.000 description 2
- 229940095074 cyclic amp Drugs 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- 238000011156 evaluation Methods 0.000 description 2
- 235000019253 formic acid Nutrition 0.000 description 2
- 230000006870 function Effects 0.000 description 2
- 102000051949 human CXCL9 Human genes 0.000 description 2
- 102000049118 human CXCR5 Human genes 0.000 description 2
- 102000052080 human FFAR1 Human genes 0.000 description 2
- 102000055585 human GPER1 Human genes 0.000 description 2
- 102000049028 human GPR17 Human genes 0.000 description 2
- 102000045859 human GPR18 Human genes 0.000 description 2
- 102000057708 human GPR183 Human genes 0.000 description 2
- 102000049822 human GPR19 Human genes 0.000 description 2
- 102000055681 human GPR20 Human genes 0.000 description 2
- 102000044097 human GPR21 Human genes 0.000 description 2
- 102000050454 human GPR22 Human genes 0.000 description 2
- 102000052661 human GPR31 Human genes 0.000 description 2
- 102000055221 human GPR32 Human genes 0.000 description 2
- 102000045056 human GPR37L1 Human genes 0.000 description 2
- 102000056566 human GPR68 Human genes 0.000 description 2
- 102000044989 human HCAR3 Human genes 0.000 description 2
- 102000055497 human NPBWR2 Human genes 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 210000000265 leukocyte Anatomy 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- KWGKDLIKAYFUFQ-UHFFFAOYSA-M lithium chloride Chemical compound [Li+].[Cl-] KWGKDLIKAYFUFQ-UHFFFAOYSA-M 0.000 description 2
- 238000004020 luminiscence type Methods 0.000 description 2
- 210000003563 lymphoid tissue Anatomy 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 210000002569 neuron Anatomy 0.000 description 2
- 210000000496 pancreas Anatomy 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- 230000001737 promoting effect Effects 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 230000019491 signal transduction Effects 0.000 description 2
- 235000010339 sodium tetraborate Nutrition 0.000 description 2
- 230000006641 stabilisation Effects 0.000 description 2
- 238000011105 stabilization Methods 0.000 description 2
- 230000004936 stimulating effect Effects 0.000 description 2
- 230000000638 stimulation Effects 0.000 description 2
- 230000005062 synaptic transmission Effects 0.000 description 2
- 210000001550 testis Anatomy 0.000 description 2
- 210000001685 thyroid gland Anatomy 0.000 description 2
- 238000010361 transduction Methods 0.000 description 2
- 230000026683 transduction Effects 0.000 description 2
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 2
- BSVBQGMMJUBVOD-UHFFFAOYSA-N trisodium borate Chemical compound [Na+].[Na+].[Na+].[O-]B([O-])[O-] BSVBQGMMJUBVOD-UHFFFAOYSA-N 0.000 description 2
- 238000005406 washing Methods 0.000 description 2
- UHDGCWIWMRVCDJ-UHFFFAOYSA-N 1-beta-D-Xylofuranosyl-NH-Cytosine Natural products O=C1N=C(N)C=CN1C1C(O)C(O)C(CO)O1 UHDGCWIWMRVCDJ-UHFFFAOYSA-N 0.000 description 1
- 125000001572 5'-adenylyl group Chemical group C=12N=C([H])N=C(N([H])[H])C=1N=C([H])N2[C@@]1([H])[C@@](O[H])([H])[C@@](O[H])([H])[C@](C(OP(=O)(O[H])[*])([H])[H])([H])O1 0.000 description 1
- 108010072564 5-HT2A Serotonin Receptor Proteins 0.000 description 1
- 102000049773 5-HT2A Serotonin Receptor Human genes 0.000 description 1
- 102000006902 5-HT2C Serotonin Receptor Human genes 0.000 description 1
- 108010072553 5-HT2C Serotonin Receptor Proteins 0.000 description 1
- 101710138091 5-hydroxytryptamine receptor 2A Proteins 0.000 description 1
- 102100036321 5-hydroxytryptamine receptor 2A Human genes 0.000 description 1
- 102220574386 5-hydroxytryptamine receptor 2A_T25N_mutation Human genes 0.000 description 1
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 description 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 description 1
- 102100024402 Alpha-1B adrenergic receptor Human genes 0.000 description 1
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- DWRXFEITVBNRMK-UHFFFAOYSA-N Beta-D-1-Arabinofuranosylthymine Natural products O=C1NC(=O)C(C)=CN1C1C(O)C(O)C(CO)O1 DWRXFEITVBNRMK-UHFFFAOYSA-N 0.000 description 1
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 1
- 239000002126 C01EB10 - Adenosine Substances 0.000 description 1
- 101100291255 Caenorhabditis elegans mig-39 gene Proteins 0.000 description 1
- 102000000844 Cell Surface Receptors Human genes 0.000 description 1
- 108010001857 Cell Surface Receptors Proteins 0.000 description 1
- 108020004638 Circular DNA Proteins 0.000 description 1
- 102000004420 Creatine Kinase Human genes 0.000 description 1
- 108010042126 Creatine kinase Proteins 0.000 description 1
- MIKUYHXYGGJMLM-GIMIYPNGSA-N Crotonoside Natural products C1=NC2=C(N)NC(=O)N=C2N1[C@H]1O[C@@H](CO)[C@H](O)[C@@H]1O MIKUYHXYGGJMLM-GIMIYPNGSA-N 0.000 description 1
- 101710095468 Cyclase Proteins 0.000 description 1
- UHDGCWIWMRVCDJ-PSQAKQOGSA-N Cytidine Natural products O=C1N=C(N)C=CN1[C@@H]1[C@@H](O)[C@@H](O)[C@H](CO)O1 UHDGCWIWMRVCDJ-PSQAKQOGSA-N 0.000 description 1
- NYHBQMYGNKIUIF-UHFFFAOYSA-N D-guanosine Natural products C1=2NC(N)=NC(=O)C=2N=CN1C1OC(CO)C(O)C1O NYHBQMYGNKIUIF-UHFFFAOYSA-N 0.000 description 1
- 238000002965 ELISA Methods 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 102100033012 G-protein coupled receptor 12 Human genes 0.000 description 1
- 102000052874 Gastrin receptors Human genes 0.000 description 1
- 102100036016 Gastrin/cholecystokinin type B receptor Human genes 0.000 description 1
- 108091006101 Gi proteins Proteins 0.000 description 1
- 102000034354 Gi proteins Human genes 0.000 description 1
- 239000004471 Glycine Substances 0.000 description 1
- 241000238631 Hexapoda Species 0.000 description 1
- 101001015106 Homo sapiens G-protein coupled receptor 12 Proteins 0.000 description 1
- 101001116388 Homo sapiens Melatonin-related receptor Proteins 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 description 1
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 description 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 1
- 102000018697 Membrane Proteins Human genes 0.000 description 1
- 108010052285 Membrane Proteins Proteins 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 108091005461 Nucleic proteins Proteins 0.000 description 1
- 108700026244 Open Reading Frames Proteins 0.000 description 1
- 101150037263 PIP2 gene Proteins 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 108010002747 Pfu DNA polymerase Proteins 0.000 description 1
- BELBBZDIHDAJOR-UHFFFAOYSA-N Phenolsulfonephthalein Chemical compound C1=CC(O)=CC=C1C1(C=2C=CC(O)=CC=2)C2=CC=CC=C2S(=O)(=O)O1 BELBBZDIHDAJOR-UHFFFAOYSA-N 0.000 description 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 description 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 101000633010 Rattus norvegicus Somatostatin Proteins 0.000 description 1
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 1
- 101100262439 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) UBA2 gene Proteins 0.000 description 1
- 108010006785 Taq Polymerase Proteins 0.000 description 1
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 description 1
- 239000004473 Threonine Substances 0.000 description 1
- 239000007983 Tris buffer Substances 0.000 description 1
- YZCKVEUIGOORGS-NJFSPNSNSA-N Tritium Chemical compound [3H] YZCKVEUIGOORGS-NJFSPNSNSA-N 0.000 description 1
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Chemical compound CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 description 1
- 241000700605 Viruses Species 0.000 description 1
- 108010046516 Wheat Germ Agglutinins Proteins 0.000 description 1
- 125000005426 adeninyl group Chemical group N1=C(N=C2N=CNC2=C1N)* 0.000 description 1
- 229960005305 adenosine Drugs 0.000 description 1
- 239000011543 agarose gel Substances 0.000 description 1
- 108020004102 alpha-1 Adrenergic Receptor Proteins 0.000 description 1
- VZTDIZULWFCMLS-UHFFFAOYSA-N ammonium formate Chemical compound [NH4+].[O-]C=O VZTDIZULWFCMLS-UHFFFAOYSA-N 0.000 description 1
- 239000003957 anion exchange resin Substances 0.000 description 1
- 235000009582 asparagine Nutrition 0.000 description 1
- 229960001230 asparagine Drugs 0.000 description 1
- 235000003704 aspartic acid Nutrition 0.000 description 1
- 238000000376 autoradiography Methods 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- WQZGKKKJIJFFOK-FPRJBGLDSA-N beta-D-galactose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-FPRJBGLDSA-N 0.000 description 1
- IQFYYKKMVGJFEH-UHFFFAOYSA-N beta-L-thymidine Natural products O=C1NC(=O)C(C)=CN1C1OC(CO)C(O)C1 IQFYYKKMVGJFEH-UHFFFAOYSA-N 0.000 description 1
- DRTQHJPVMGBUCF-PSQAKQOGSA-N beta-L-uridine Natural products O[C@H]1[C@@H](O)[C@H](CO)O[C@@H]1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-PSQAKQOGSA-N 0.000 description 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 1
- 239000012148 binding buffer Substances 0.000 description 1
- 230000008512 biological response Effects 0.000 description 1
- 230000003491 cAMP production Effects 0.000 description 1
- 230000020411 cell activation Effects 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 108091092356 cellular DNA Proteins 0.000 description 1
- 210000001638 cerebellum Anatomy 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 238000001311 chemical methods and process Methods 0.000 description 1
- 238000007385 chemical modification Methods 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 238000012790 confirmation Methods 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 235000018417 cysteine Nutrition 0.000 description 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 description 1
- UHDGCWIWMRVCDJ-ZAKLUEHWSA-N cytidine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O1 UHDGCWIWMRVCDJ-ZAKLUEHWSA-N 0.000 description 1
- 230000001086 cytosolic effect Effects 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 238000009509 drug development Methods 0.000 description 1
- 238000001962 electrophoresis Methods 0.000 description 1
- 230000005713 exacerbation Effects 0.000 description 1
- 210000001723 extracellular space Anatomy 0.000 description 1
- 239000012091 fetal bovine serum Substances 0.000 description 1
- 239000012467 final product Substances 0.000 description 1
- 108020001507 fusion proteins Proteins 0.000 description 1
- 102000037865 fusion proteins Human genes 0.000 description 1
- 230000008303 genetic mechanism Effects 0.000 description 1
- 235000013922 glutamic acid Nutrition 0.000 description 1
- 239000004220 glutamic acid Substances 0.000 description 1
- 125000000291 glutamic acid group Chemical group N[C@@H](CCC(O)=O)C(=O)* 0.000 description 1
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 description 1
- PCHJSUWPFVWCPO-UHFFFAOYSA-N gold Chemical compound [Au] PCHJSUWPFVWCPO-UHFFFAOYSA-N 0.000 description 1
- 239000010931 gold Substances 0.000 description 1
- 229910052737 gold Inorganic materials 0.000 description 1
- 230000012010 growth Effects 0.000 description 1
- 239000001963 growth medium Substances 0.000 description 1
- 229940029575 guanosine Drugs 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 210000001320 hippocampus Anatomy 0.000 description 1
- 238000000265 homogenisation Methods 0.000 description 1
- 102000047215 human APLNR Human genes 0.000 description 1
- 102000043824 human FFAR3 Human genes 0.000 description 1
- 102000005294 human G-protein coupled receptor 43 Human genes 0.000 description 1
- 102000052820 human GPR1 Human genes 0.000 description 1
- 102000044101 human GPR4 Human genes 0.000 description 1
- 102000047277 human MCHR1 Human genes 0.000 description 1
- 102000056662 human NPBWR1 Human genes 0.000 description 1
- 238000003119 immunoblot Methods 0.000 description 1
- 238000007901 in situ hybridization Methods 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 description 1
- 229960000310 isoleucine Drugs 0.000 description 1
- 238000005304 joining Methods 0.000 description 1
- FPCCSQOGAWCVBH-UHFFFAOYSA-N ketanserin Chemical compound C1=CC(F)=CC=C1C(=O)C1CCN(CCN2C(C3=CC=CC=C3NC2=O)=O)CC1 FPCCSQOGAWCVBH-UHFFFAOYSA-N 0.000 description 1
- 229960005417 ketanserin Drugs 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 238000002372 labelling Methods 0.000 description 1
- 230000001926 lymphatic effect Effects 0.000 description 1
- 239000006166 lysate Substances 0.000 description 1
- 125000003588 lysine group Chemical group [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 description 1
- 210000005075 mammary gland Anatomy 0.000 description 1
- 238000000691 measurement method Methods 0.000 description 1
- 230000007721 medicinal effect Effects 0.000 description 1
- 229930182817 methionine Natural products 0.000 description 1
- 230000003278 mimic effect Effects 0.000 description 1
- 238000006386 neutralization reaction Methods 0.000 description 1
- 239000002777 nucleoside Substances 0.000 description 1
- 150000003833 nucleoside derivatives Chemical class 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 210000001672 ovary Anatomy 0.000 description 1
- 239000011049 pearl Substances 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 239000008177 pharmaceutical agent Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 229960003531 phenolsulfonphthalein Drugs 0.000 description 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 description 1
- 235000021317 phosphate Nutrition 0.000 description 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 150000003013 phosphoric acid derivatives Chemical class 0.000 description 1
- 230000026731 phosphorylation Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- 230000004962 physiological condition Effects 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 239000000955 prescription drug Substances 0.000 description 1
- 210000002637 putamen Anatomy 0.000 description 1
- 230000002285 radioactive effect Effects 0.000 description 1
- 239000000018 receptor agonist Substances 0.000 description 1
- 229940044601 receptor agonist Drugs 0.000 description 1
- 230000010076 replication Effects 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- 108091008146 restriction endonucleases Proteins 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 102200121669 rs104894915 Human genes 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 238000002864 sequence alignment Methods 0.000 description 1
- 238000012163 sequencing technique Methods 0.000 description 1
- 239000012679 serum free medium Substances 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 235000019254 sodium formate Nutrition 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 210000000278 spinal cord Anatomy 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 229940104230 thymidine Drugs 0.000 description 1
- 230000009261 transgenic effect Effects 0.000 description 1
- 102000027257 transmembrane receptors Human genes 0.000 description 1
- 108091008578 transmembrane receptors Proteins 0.000 description 1
- 239000001226 triphosphate Substances 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
- 241000701161 unidentified adenovirus Species 0.000 description 1
- DRTQHJPVMGBUCF-UHFFFAOYSA-N uracil arabinoside Natural products OC1C(O)C(CO)OC1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-UHFFFAOYSA-N 0.000 description 1
- 229940045145 uridine Drugs 0.000 description 1
- 125000002987 valine group Chemical group [H]N([H])C([H])(C(*)=O)C([H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 210000005253 yeast cell Anatomy 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
- C07K14/72—Receptors; Cell surface antigens; Cell surface determinants for hormones
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/16—Halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
- C07K14/70571—Receptors; Cell surface antigens; Cell surface determinants for neuromediators, e.g. serotonin receptor, dopamine receptor
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
- C07K14/72—Receptors; Cell surface antigens; Cell surface determinants for hormones
- C07K14/723—G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH receptor
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
- G01N33/566—Immunoassay; Biospecific binding assay; Materials therefor using specific carrier or receptor proteins as ligand binding reagents where possible specific carrier or receptor proteins are classified with their target compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
- G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
- G01N2333/72—Assays involving receptors, cell surface antigens or cell surface determinants for hormones
- G01N2333/726—G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2500/00—Screening for compounds of potential therapeutic value
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Immunology (AREA)
- Molecular Biology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Cell Biology (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Physics & Mathematics (AREA)
- Microbiology (AREA)
- Pathology (AREA)
- General Physics & Mathematics (AREA)
- Analytical Chemistry (AREA)
- Neurology (AREA)
- Food Science & Technology (AREA)
- Biotechnology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Peptides Or Proteins (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/170,496 US6555339B1 (en) | 1997-04-14 | 1998-10-13 | Non-endogenous, constitutively activated human protein-coupled receptors |
| US170496 | 1998-10-13 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ES2163384T1 ES2163384T1 (es) | 2002-02-01 |
| ES2163384T3 true ES2163384T3 (es) | 2006-12-01 |
Family
ID=22620080
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES99951991T Expired - Lifetime ES2163384T3 (es) | 1998-10-13 | 1999-10-12 | Receptores acoplados a proteinas g humanos, activados de forma constitutiva, no endogenos. |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US6555339B1 (enExample) |
| EP (1) | EP1121431B9 (enExample) |
| JP (2) | JP4672866B2 (enExample) |
| KR (1) | KR100598752B1 (enExample) |
| CN (1) | CN1329511C (enExample) |
| AT (1) | ATE318311T1 (enExample) |
| AU (5) | AU769987B2 (enExample) |
| CA (1) | CA2342314A1 (enExample) |
| DE (3) | DE1121431T1 (enExample) |
| DK (1) | DK1121431T5 (enExample) |
| ES (1) | ES2163384T3 (enExample) |
| IL (2) | IL141965A0 (enExample) |
| NZ (1) | NZ510331A (enExample) |
| WO (2) | WO2000021987A2 (enExample) |
Families Citing this family (172)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7888466B2 (en) | 1996-01-11 | 2011-02-15 | Human Genome Sciences, Inc. | Human G-protein chemokine receptor HSATU68 |
| US6555339B1 (en) * | 1997-04-14 | 2003-04-29 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated human protein-coupled receptors |
| US7816492B2 (en) * | 1998-11-20 | 2010-10-19 | Arena Pharmaceuticals, Inc. | Human G protein-coupled receptors |
| USRE42190E1 (en) | 1998-11-20 | 2011-03-01 | Arena Pharmaceuticals, Inc. | Method of identifying a compound for inhibiting or stimulating human G protein-coupled receptors |
| US20030017528A1 (en) | 1998-11-20 | 2003-01-23 | Ruoping Chen | Human orphan G protein-coupled receptors |
| PT1133559E (pt) * | 1998-11-20 | 2005-10-31 | Arena Pharm Inc | Receptor acoplato a proteina g orfao humano, rup3 |
| GB9903767D0 (en) * | 1999-02-18 | 1999-04-14 | Univ Glasgow | Receptor assay |
| AU6385200A (en) * | 1999-07-30 | 2001-02-19 | Millennium Pharmaceuticals, Inc. | Compositions, kits, and methods for prognostication, diagnosis, prevention, and treatment of bone-related disorders and other disorders |
| JP4768946B2 (ja) * | 1999-11-17 | 2011-09-07 | アリーナ ファーマシューティカルズ， インコーポレイテッド | ヒトｇタンパク質共役型受容体の内因性および非内因性型 |
| EP1240199A2 (en) * | 1999-12-10 | 2002-09-18 | AstraZeneca AB | Method for screening of appetite control agents |
| JP2003517008A (ja) * | 1999-12-17 | 2003-05-20 | アストラゼネカ アクチボラグ | 新規化合物 |
| AU2001232132A1 (en) * | 2000-02-18 | 2001-08-27 | Glaxo Group Limited | Novel assay |
| GB0003902D0 (en) * | 2000-02-18 | 2000-04-05 | Glaxo Group Ltd | Assay |
| GB0003898D0 (en) * | 2000-02-18 | 2000-04-05 | Glaxo Group Ltd | Assay |
| WO2001064872A2 (en) * | 2000-02-29 | 2001-09-07 | Millennium Pharmaceuticals, Inc. | Gene 2465: methods and compositions for the diagnosis and treatment of cardiovascular, hepatic and bone disease |
| US6436703B1 (en) * | 2000-03-31 | 2002-08-20 | Hyseq, Inc. | Nucleic acids and polypeptides |
| EP1278850B1 (en) * | 2000-04-26 | 2007-06-13 | Sanofi-Aventis Deutschland GmbH | Edg8 receptor, its preparation and use |
| EP1149907A1 (en) * | 2000-04-26 | 2001-10-31 | Aventis Pharma Deutschland GmbH | EDG8 receptor, its preparation and use |
| AU2001250536A1 (en) * | 2000-05-03 | 2001-11-12 | Astrazeneca Ab | Methods |
| AU2001274522A1 (en) * | 2000-06-15 | 2001-12-24 | Takeda Chemical Industries Ltd. | Novel g protein-coupled receptor protein and dna thereof |
| EP1297130A2 (en) * | 2000-06-16 | 2003-04-02 | Incyte Genomics, Inc. | G-protein coupled receptors |
| WO2001098494A1 (fr) * | 2000-06-21 | 2001-12-27 | Takeda Chemical Industries, Ltd | Ligand de gpr8 et son adn |
| US20040086940A1 (en) * | 2000-07-04 | 2004-05-06 | Sachio Shibata | Novel g protein-coupled receptor protein and dna thereof |
| WO2002013845A2 (en) * | 2000-08-18 | 2002-02-21 | Novartis Ag | Inflammation related g-protein coupled receptor |
| AU2001286945A1 (en) * | 2000-08-30 | 2002-03-13 | John Hopkins University School Of Medicine | Identification of activated receptors and ion channels |
| AU2000276780A1 (en) * | 2000-10-02 | 2001-04-23 | Biofocus Discovery Limited | Cellular receptor mutations predicted by multiple-sequence-allignment |
| EP1344823A4 (en) * | 2000-11-30 | 2005-03-16 | Takeda Chemical Industries Ltd | NEW G-PROTEIN-COUPLED RECEPTOR PROTEINS AND THEIR DNAS |
| US7241579B2 (en) | 2000-12-22 | 2007-07-10 | Smithkline Beecham Corporation | Method of screening for GPR40 ligands |
| GB0031527D0 (en) * | 2000-12-22 | 2001-02-07 | Smithkline Beecham Plc | New use |
| CN1516706A (zh) * | 2001-02-26 | 2004-07-28 | 阿伦纳药品公司 | 人g蛋白偶联受体的内源性和非内源性形式 |
| US6809104B2 (en) | 2001-05-04 | 2004-10-26 | Tularik Inc. | Fused heterocyclic compounds |
| US6919176B2 (en) * | 2001-05-07 | 2005-07-19 | Amgen Inc. | Polypeptides and nucleic acids associated with cancer |
| EP1394543B1 (en) * | 2001-05-15 | 2007-08-29 | Takeda Pharmaceutical Company Limited | Screening method |
| US20020177190A1 (en) * | 2001-05-24 | 2002-11-28 | Yanbin Liang | Recombinant simian GPR3 receptor |
| CA2449553A1 (en) * | 2001-06-05 | 2002-12-19 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated versions of plant g protein-coupled receptor: gcr1 |
| JP2003018992A (ja) * | 2001-06-28 | 2003-01-21 | Inst Of Physical & Chemical Res | Ｐａｅｌ受容体、Ｐａｅｌ受容体発現細胞および動物、ならびにパーキンソン病治療薬のスクリーニング法 |
| US20050142548A1 (en) * | 2001-07-13 | 2005-06-30 | Thomson Anne M. | Allelic variants of grp50 |
| US20030109044A1 (en) * | 2001-10-16 | 2003-06-12 | Millennium Pharmaceuticals, Inc. | Methods of using 279, a human G protein-coupled protein receptor |
| US20030119742A1 (en) * | 2001-11-05 | 2003-06-26 | Millennium Pharmaceuticals, Inc. | Methods and compositions to treat cardiovascular disease using 139, 258, 1261, 1486, 2398, 2414, 7660, 8587,10183, 10550, 12680, 17921, 32248, 60489 or 93804 |
| US6902902B2 (en) | 2001-11-27 | 2005-06-07 | Arena Pharmaceuticals, Inc. | Human G protein-coupled receptors and modulators thereof for the treatment of metabolic-related disorders |
| EP1463759B8 (en) | 2002-01-07 | 2013-07-10 | Euroscreen S.A. | Ligand for g-protein coupled receptor gpr43 and uses thereof |
| EP1336655A1 (en) * | 2002-01-12 | 2003-08-20 | Aventis Pharma Deutschland GmbH | Method of identifying protein CAMS (constitutively active mutants) |
| US20030175889A1 (en) * | 2002-01-23 | 2003-09-18 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated versions of human G protein coupled receptor: FSHR |
| JP2005534282A (ja) * | 2002-02-06 | 2005-11-17 | バイエル・ヘルスケア・アクチェンゲゼルシャフト | ニューロメジンｕ受容体に関連する疾患のための診断用および治療用物質 |
| US7214495B2 (en) | 2002-02-14 | 2007-05-08 | Takeda Pharmaceutical Company Limited | Screening method |
| AU2003218234A1 (en) * | 2002-03-15 | 2003-09-29 | Arena Pharmaceuticals, Inc. | Methods of expressing non-endogenous g protein coupled receptors in cells |
| AU2003241037A1 (en) * | 2002-06-08 | 2003-12-22 | Astrazeneca Ab | Methods for the detection of polymorphisms in human gpr50 |
| CN100473662C (zh) * | 2002-08-01 | 2009-04-01 | 阿瑞那制药公司 | 治疗缺血性心脏病及充血性心衰竭的人类g蛋白偶联受体及其调节物 |
| WO2004015426A1 (en) * | 2002-08-06 | 2004-02-19 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with human cxc chemokine receptor 5(cxcr5) |
| AU2003250165A1 (en) * | 2002-08-06 | 2004-02-25 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with g-protein coupled receptor 19 (gpr19) |
| WO2004017994A1 (ja) * | 2002-08-22 | 2004-03-04 | Kyowa Hakko Kogyo Co., Ltd. | 喘息の予防および／または治療剤 |
| WO2004038407A2 (en) * | 2002-10-24 | 2004-05-06 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with human g-protein coupled receptor 12 (gpr12) |
| US7056685B1 (en) | 2002-11-05 | 2006-06-06 | Amgen Inc. | Receptor ligands and methods of modulating receptors |
| PL376659A1 (pl) | 2002-11-06 | 2006-01-09 | Tularik Inc. | Skondensowane związki heterocykliczne |
| US7960369B2 (en) | 2002-11-08 | 2011-06-14 | Takeda Pharmaceutical Company Limited | Receptor function regulator |
| US7189524B1 (en) | 2002-11-25 | 2007-03-13 | Amgen, Inc. | Receptor ligands and methods of modulating receptors |
| WO2004050853A2 (en) * | 2002-12-04 | 2004-06-17 | Synaptic Pharmaceutical Corporation | Uses of the snorf55 receptor |
| US20040157253A1 (en) * | 2003-02-07 | 2004-08-12 | Millennium Pharmaceuticals, Inc. | Methods and compositions for use of inflammatory proteins in the diagnosis and treatment of metabolic disorders |
| WO2004083388A2 (en) * | 2003-03-14 | 2004-09-30 | Bristol-Myers Squibb Company | Polynucleotide encoding a novel human g-protein coupled receptor variant of hm74, hgprbmy74 |
| WO2004083394A2 (en) * | 2003-03-18 | 2004-09-30 | Arena Pharmaceuticals Inc. | Human g protein-coupled receptors and modulators thereof for the treatment of inflammatory disorders |
| JPWO2004093912A1 (ja) * | 2003-04-23 | 2006-07-13 | 協和醗酵工業株式会社 | 好中球性炎症疾患の予防および／または治療剤 |
| WO2004099419A2 (en) * | 2003-04-30 | 2004-11-18 | Arena Pharmaceuticals, Inc. | Methods and compositions for identifying modulators of g protein-coupled receptors |
| EP1625159B1 (en) * | 2003-05-20 | 2011-03-02 | The University Court Of The University Of Glasgow | Materials and methods relating to g-protein coupled receptor oligomers |
| EP1666880B1 (en) * | 2003-09-11 | 2008-08-20 | Takeda Pharmaceutical Company Limited | Screening method |
| US20070276024A1 (en) * | 2003-10-09 | 2007-11-29 | Inverseon , Inc. | Methods for Treating Diseases and Conditions with Inverse Agonists and for Screening for Agents Acting as Inverse Agonists |
| AU2004280638A1 (en) * | 2003-10-09 | 2005-04-21 | Inverseon, Inc. | Methods for treating diseases and conditions with inverse agonists and for screening for agents acting as inverse agonists |
| WO2005040829A2 (en) * | 2003-10-21 | 2005-05-06 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with g protein-coupled receptor 17 (gpr17) |
| WO2005040211A2 (en) * | 2003-10-23 | 2005-05-06 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with g protein-coupled receptor 1 (gpr1) |
| WO2005040828A2 (en) * | 2003-10-24 | 2005-05-06 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with g protein-coupled receptor 49 (gpr49) |
| WO2005040825A2 (en) * | 2003-10-24 | 2005-05-06 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with g protein-coupled receptor 20 (gpr20) |
| NZ583292A (en) | 2003-11-06 | 2012-03-30 | Seattle Genetics Inc | Monomethylvaline compounds capable of conjugation to ligands |
| DK1713501T3 (da) * | 2004-01-29 | 2008-05-26 | Cellzome Ag | Behandling af neurodegenerative sygdomme ved anvendelse af GPR49 |
| EP1718293A1 (en) | 2004-02-20 | 2006-11-08 | Aventis Pharmaceuticals Inc. | Oxydecahydronaphthalene modulators of hm74 |
| WO2005101005A1 (en) * | 2004-04-15 | 2005-10-27 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with g-protein coupled receptor 32 (gpr32) |
| ATE486962T1 (de) * | 2004-04-27 | 2010-11-15 | Takeda Pharmaceutical | Neuer ligand eines g-protein-konjugierten rezeptorproteins und verwendung davon |
| MXPA06014065A (es) | 2004-06-01 | 2007-01-31 | Genentech Inc | Conjugados de droga-anticuerpo y metodos. |
| US20100111856A1 (en) | 2004-09-23 | 2010-05-06 | Herman Gill | Zirconium-radiolabeled, cysteine engineered antibody conjugates |
| ES2579805T3 (es) | 2004-09-23 | 2016-08-16 | Genentech, Inc. | Anticuerpos y conjugados modificados por ingeniería genética con cisteína |
| US7528175B2 (en) * | 2004-10-08 | 2009-05-05 | Inverseon, Inc. | Method of treating airway diseases with beta-adrenergic inverse agonists |
| GB0508988D0 (en) | 2005-05-03 | 2005-06-08 | Novartis Ag | Organic compounds |
| US8429755B2 (en) | 2005-05-26 | 2013-04-23 | Sandisk Technologies Inc. | System and method for receiving digital content |
| US8673848B2 (en) | 2012-01-27 | 2014-03-18 | Novartis Ag | Synthetic apelin mimetics for the treatment of heart failure |
| US20090313708A1 (en) * | 2005-10-14 | 2009-12-17 | Liaw Chen W | Gpr22 and methods relating thereto |
| WO2007058930A1 (en) | 2005-11-10 | 2007-05-24 | Arena Pharmaceuticals, Inc. | Human g protein-coupled receptor and modulators thereof for the treatment of obesity and conditions related thereto |
| CN101688203B (zh) | 2007-03-22 | 2013-12-11 | 赫普泰雅治疗有限公司 | 突变的g蛋白偶联受体及其选择方法 |
| GB0724051D0 (en) | 2007-12-08 | 2008-01-16 | Medical Res Council | Mutant proteins and methods for producing them |
| GB0724860D0 (en) | 2007-12-20 | 2008-01-30 | Heptares Therapeutics Ltd | Screening |
| GB0802474D0 (en) | 2008-02-11 | 2008-03-19 | Heptares Therapeutics Ltd | Mutant proteins and methods for selecting them |
| EP2146210A1 (en) | 2008-04-07 | 2010-01-20 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY |
| WO2010091692A2 (en) * | 2009-04-30 | 2010-08-19 | H. Lundbeck A/S | Constitutively active mutants and uses thereof |
| GB0910725D0 (en) | 2009-06-22 | 2009-08-05 | Heptares Therapeutics Ltd | Mutant proteins and methods for producing them |
| CA2809819A1 (en) | 2009-09-09 | 2011-03-17 | Centrose, Llc | Extracellular targeted drug conjugates |
| US20110256157A1 (en) | 2010-04-15 | 2011-10-20 | Spirogen Limited | Pyrrolobenzodiazepines and conjugates thereof |
| JP2013534520A (ja) | 2010-06-08 | 2013-09-05 | ジェネンテック， インコーポレイテッド | システイン操作抗体及びコンジュゲート |
| JP5804341B2 (ja) * | 2010-08-06 | 2015-11-04 | 国立大学法人山口大学 | エストロゲン関連疾患の判定方法 |
| ES2544608T3 (es) | 2010-11-17 | 2015-09-02 | Genentech, Inc. | Conjugados de anticuerpo y de alaninil-maitansinol |
| CA2833212C (en) | 2011-05-12 | 2020-06-09 | Genentech, Inc. | Multiple reaction monitoring lc-ms/ms method to detect therapeutic antibodies in animal samples using framework signature peptides |
| HRP20151374T1 (hr) | 2011-10-14 | 2016-01-15 | Medimmune Limited | Pirolobenzodiazepini i njihovi konjugati |
| WO2013130093A1 (en) | 2012-03-02 | 2013-09-06 | Genentech, Inc. | Biomarkers for treatment with anti-tubulin chemotherapeutic compounds |
| JP6392764B2 (ja) | 2012-10-12 | 2018-09-19 | エイディーシー・セラピューティクス・エス・アーＡｄｃ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｓａ | ピロロベンゾジアゼピン−抗体結合体 |
| HUE045435T2 (hu) | 2012-10-12 | 2019-12-30 | Medimmune Ltd | Pirrolobenzodiazepinek és konjugátumaik |
| EP2906250B1 (en) | 2012-10-12 | 2018-05-30 | ADC Therapeutics SA | Pyrrolobenzodiazepine-anti-psma antibody conjugates |
| JP6270859B2 (ja) | 2012-10-12 | 2018-01-31 | エイディーシー・セラピューティクス・エス・アー・エール・エルＡｄｃ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｓａｒｌ | ピロロベンゾジアゼピン−抗体結合体 |
| LT2906251T (lt) | 2012-10-12 | 2017-12-11 | Adc Therapeutics Sa | Pirolobenzodiazepino-anti-cd22 antikūno konjugatai |
| HRP20182129T1 (hr) | 2012-10-12 | 2019-02-08 | Adc Therapeutics Sa | Konjugati protutijelo - pirolobenzodiazepin |
| EP2906297B1 (en) | 2012-10-12 | 2017-12-06 | ADC Therapeutics SA | Pyrrolobenzodiazepine-antibody conjugates |
| US8921307B2 (en) | 2012-11-20 | 2014-12-30 | Novartis Ag | Synthetic linear apelin mimetics for the treatment of heart failure |
| UY35144A (es) | 2012-11-20 | 2014-06-30 | Novartis Ag | Miméticos lineales sintéticos de apelina para el tratamiento de insuficiencia cardiaca |
| US9567340B2 (en) | 2012-12-21 | 2017-02-14 | Medimmune Limited | Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases |
| AU2013366493B2 (en) | 2012-12-21 | 2017-08-24 | Medimmune Limited | Pyrrolobenzodiazepines and conjugates thereof |
| CN105307685B (zh) | 2013-03-13 | 2019-03-08 | 麦迪穆有限责任公司 | 吡咯并苯并二氮杂卓和其结合物 |
| JP6444902B2 (ja) | 2013-03-13 | 2018-12-26 | メドイミューン・リミテッドＭｅｄＩｍｍｕｎｅ Ｌｉｍｉｔｅｄ | ピロロベンゾジアゼピン及びその結合体 |
| CA2904044C (en) | 2013-03-13 | 2020-03-31 | Medimmune Limited | Pyrrolobenzodiazepines and conjugates thereof |
| TW201518323A (zh) | 2013-07-25 | 2015-05-16 | Novartis Ag | 合成ａｐｅｌｉｎ多肽之生物結合物 |
| SG11201600211XA (en) | 2013-07-25 | 2016-02-26 | Novartis Ag | Cyclic polypeptides for the treatment of heart failure |
| MX2016001862A (es) | 2013-08-12 | 2016-08-03 | Genentech Inc | Compuestos de conjugado anticuerpo-farmaco dimerico de 1-(clorometil)-2,3-dihidro-1h-benzo[e]indol, y metodos de uso y tratamiento. |
| WO2015052532A1 (en) | 2013-10-11 | 2015-04-16 | Spirogen Sàrl | Pyrrolobenzodiazepine-antibody conjugates |
| GB201317982D0 (en) | 2013-10-11 | 2013-11-27 | Spirogen Sarl | Pyrrolobenzodiazepines and conjugates thereof |
| US9950078B2 (en) | 2013-10-11 | 2018-04-24 | Medimmune Limited | Pyrrolobenzodiazepine-antibody conjugates |
| US9956299B2 (en) | 2013-10-11 | 2018-05-01 | Medimmune Limited | Pyrrolobenzodiazepine—antibody conjugates |
| AU2014364927A1 (en) | 2013-12-16 | 2016-07-07 | Genentech, Inc. | Peptidomimetic compounds and antibody-drug conjugates thereof |
| EP3082874A2 (en) | 2013-12-16 | 2016-10-26 | Genentech, Inc. | Peptidomimetic compounds and antibody-drug conjugates thereof |
| JP6980384B2 (ja) | 2013-12-16 | 2021-12-15 | ジェネンテック， インコーポレイテッド | １−（クロロメチル）−２，３−ジヒドロ−１ｈ−ベンゾ［ｅ］インドール二量体抗体−薬物コンジュゲート化合物、並びに使用及び処置の方法 |
| CA2945706C (en) * | 2014-04-25 | 2023-10-24 | Libramen Naturals Inc. | G-protein coupled receptor 22 transformed cell lines and uses therefor |
| JP6531166B2 (ja) | 2014-09-10 | 2019-06-12 | メドイミューン・リミテッドＭｅｄＩｍｍｕｎｅ Ｌｉｍｉｔｅｄ | ピロロベンゾジアゼピン及びそのコンジュゲート |
| GB201416112D0 (en) | 2014-09-12 | 2014-10-29 | Medimmune Ltd | Pyrrolobenzodiazepines and conjugates thereof |
| JP6622293B2 (ja) | 2014-09-12 | 2019-12-18 | ジェネンテック， インコーポレイテッド | アントラサイクリンジスルフィド中間体、抗体−薬物複合体、及び方法 |
| AU2015314826A1 (en) | 2014-09-12 | 2017-03-02 | Genentech, Inc. | Cysteine engineered antibodies and conjugates |
| CA2959689A1 (en) | 2014-09-17 | 2016-03-24 | Genentech, Inc. | Pyrrolobenzodiazepines and antibody disulfide conjugates thereof |
| EP3223854A1 (en) | 2014-11-25 | 2017-10-04 | ADC Therapeutics SA | Pyrrolobenzodiazepine-antibody conjugates |
| KR20170086121A (ko) | 2014-12-03 | 2017-07-25 | 제넨테크, 인크. | 4급 아민 화합물 및 그의 항체-약물 접합체 |
| GB201506411D0 (en) | 2015-04-15 | 2015-05-27 | Bergenbio As | Humanized anti-axl antibodies |
| GB201506402D0 (en) | 2015-04-15 | 2015-05-27 | Berkel Patricius H C Van And Howard Philip W | Site-specific antibody-drug conjugates |
| MA43345A (fr) | 2015-10-02 | 2018-08-08 | Hoffmann La Roche | Conjugués anticorps-médicaments de pyrrolobenzodiazépine et méthodes d'utilisation |
| MA43354A (fr) | 2015-10-16 | 2018-08-22 | Genentech Inc | Conjugués médicamenteux à pont disulfure encombré |
| MA45326A (fr) | 2015-10-20 | 2018-08-29 | Genentech Inc | Conjugués calichéamicine-anticorps-médicament et procédés d'utilisation |
| GB201601431D0 (en) | 2016-01-26 | 2016-03-09 | Medimmune Ltd | Pyrrolobenzodiazepines |
| GB201602356D0 (en) | 2016-02-10 | 2016-03-23 | Medimmune Ltd | Pyrrolobenzodiazepine Conjugates |
| GB201602359D0 (en) | 2016-02-10 | 2016-03-23 | Medimmune Ltd | Pyrrolobenzodiazepine Conjugates |
| EP3416641A1 (en) | 2016-02-16 | 2018-12-26 | Deutsches Krebsforschungszentrum Stiftung des Öffentlichen Rechts | Modulators of ccr9 for treating tumor resistance to immune responses |
| EP3416640A1 (en) | 2016-02-16 | 2018-12-26 | Deutsches Krebsforschungszentrum Stiftung des Öffentlichen Rechts | Modulators of tumor immune resistance for the treatment of cancer |
| EP3433621A1 (en) | 2016-03-25 | 2019-01-30 | H. Hoffnabb-La Roche Ag | Multiplexed total antibody and antibody-conjugated drug quantification assay |
| GB201607478D0 (en) | 2016-04-29 | 2016-06-15 | Medimmune Ltd | Pyrrolobenzodiazepine Conjugates |
| PL3458101T3 (pl) | 2016-05-20 | 2021-05-31 | F. Hoffmann-La Roche Ag | Koniugaty PROTAC-przeciwciało i sposoby ich stosowania |
| WO2017205741A1 (en) | 2016-05-27 | 2017-11-30 | Genentech, Inc. | Bioanalytical method for the characterization of site-specific antibody-drug conjugates |
| CN109476648B (zh) | 2016-06-06 | 2022-09-13 | 豪夫迈·罗氏有限公司 | 司维司群抗体-药物缀合物和使用方法 |
| EP3496763A1 (en) | 2016-08-11 | 2019-06-19 | Genentech, Inc. | Pyrrolobenzodiazepine prodrugs and antibody conjugates thereof |
| EP3522933B1 (en) | 2016-10-05 | 2021-12-15 | F. Hoffmann-La Roche AG | Methods for preparing antibody drug conjugates |
| GB201617466D0 (en) | 2016-10-14 | 2016-11-30 | Medimmune Ltd | Pyrrolobenzodiazepine conjugates |
| GB201702031D0 (en) | 2017-02-08 | 2017-03-22 | Medlmmune Ltd | Pyrrolobenzodiazepine-antibody conjugates |
| KR20200032243A (ko) | 2017-02-08 | 2020-03-25 | 에이디씨 테라퓨틱스 에스에이 | 피롤로벤조디아제핀-항체 컨주게이트 |
| SI3612537T1 (sl) | 2017-04-18 | 2022-10-28 | Medimmune Limited | Konjugati pirolobenzodiazepina |
| EP3612234B1 (en) | 2017-04-20 | 2024-03-13 | ADC Therapeutics SA | Combination therapy with an anti-axl antibody-drug conjugate |
| KR102442736B1 (ko) | 2017-06-14 | 2022-09-16 | 에이디씨 테라퓨틱스 에스에이 | 항-cd19 adc의 투여를 위한 투약량 체제 |
| CN111065638B (zh) | 2017-08-18 | 2021-04-09 | 麦迪穆有限责任公司 | 吡咯并苯并二氮杂䓬缀合物 |
| CN111788208B (zh) | 2017-09-20 | 2023-11-24 | Ph制药有限公司 | 泰兰他汀类似物 |
| GB201803342D0 (en) | 2018-03-01 | 2018-04-18 | Medimmune Ltd | Methods |
| GB201806022D0 (en) | 2018-04-12 | 2018-05-30 | Medimmune Ltd | Pyrrolobenzodiazepines and conjugates thereof |
| IL296050B2 (en) | 2018-08-01 | 2024-12-01 | Immunitybio Inc | A quadricistronic system comprising a homing receptor or a cytokine, and chimeric antigen receptor for genetic modification of immunotherapies |
| GB201814281D0 (en) | 2018-09-03 | 2018-10-17 | Femtogenix Ltd | Cytotoxic agents |
| AU2019365238A1 (en) | 2018-10-24 | 2021-05-13 | F. Hoffmann-La Roche Ag | Conjugated chemical inducers of degradation and methods of use |
| WO2020123275A1 (en) | 2018-12-10 | 2020-06-18 | Genentech, Inc. | Photocrosslinking peptides for site specific conjugation to fc-containing proteins |
| GB201901197D0 (en) | 2019-01-29 | 2019-03-20 | Femtogenix Ltd | G-A Crosslinking cytotoxic agents |
| IL286326B2 (en) | 2019-03-15 | 2025-10-01 | Medimmune Ltd | Azatidobenzodiazepine dimers and conjugates containing them for use in the treatment of cancer |
| US11230699B2 (en) | 2020-01-28 | 2022-01-25 | Immunitybio, Inc. | Chimeric antigen receptor-modified NK-92 cells targeting EGFR super-family receptors |
| GB2597532A (en) | 2020-07-28 | 2022-02-02 | Femtogenix Ltd | Cytotoxic compounds |
| CA3236930A1 (en) | 2021-11-03 | 2022-04-21 | Hangzhou Dac Biotech Co., Ltd. | Specific conjugation of an antibody |
| CN114848822A (zh) * | 2022-06-01 | 2022-08-05 | 合肥工业大学 | Gpr31抑制剂在制备预防和治疗血管钙化药物中的应用 |
| WO2024044659A1 (en) * | 2022-08-24 | 2024-02-29 | Tectonic Therapeutic, Inc. | Constitutively active g protein-coupled receptor compositions and methods of use thereof |
| TW202432187A (zh) | 2022-12-23 | 2024-08-16 | 美商建南德克公司 | 小腦蛋白降解劑結合物及其用途 |
| AU2024257248A1 (en) | 2023-04-17 | 2025-11-06 | Peak Bio, Inc. | Antibodies and antibody-drug conjugates and methods of use and synthetic processes and intermediates |
| WO2025207642A1 (en) * | 2024-03-25 | 2025-10-02 | Seattle Children's Hospital D/B/A Seattle Children's Research Institute | Cxcr3 isoforms to improve recombinant receptor trafficking |
Family Cites Families (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69133064T2 (de) | 1990-02-26 | 2003-03-06 | The Board Of Trustees Of The Leland Stanford Junior University, Stanford | Identifizierung und expression von insekten-steroidrezeptor-dns-sequenzen |
| DE69232876D1 (de) | 1991-10-01 | 2003-01-30 | Us Gov Health & Human Serv | Ein verfahren zur identifikation von liganden und ligandantagonisten |
| JPH07509694A (ja) * | 1992-05-14 | 1995-10-26 | ベイラー・カレッジ・オブ・メディシン | 突然変異したステロイドホルモン受容体，その使用方法および遺伝子治療のための分子スイッチ |
| AU677968B2 (en) | 1992-09-25 | 1997-05-15 | H. Lundbeck A/S | DNA encoding human alpha 1 adrenergic receptors and uses thereof |
| EP0612845A3 (en) | 1993-02-26 | 1994-09-21 | American Cyanamid Co | Purified opioid receptor. |
| AU1173995A (en) | 1993-11-10 | 1995-05-29 | Arch Development Corporation | Ubiquitous nuclear receptor: compositions and methods |
| WO1995018380A1 (en) * | 1993-12-30 | 1995-07-06 | The Salk Institute For Biological Studies | Novel uses for gal4-receptor constructs |
| US5573944A (en) | 1994-07-22 | 1996-11-12 | President And Fellows Of Harvard College | Yeast cell expressing heterologous receptor kinase |
| EP0804575A1 (en) | 1994-08-11 | 1997-11-05 | Takeda Chemical Industries, Ltd. | G protein coupled receptor protein, production, and use thereof |
| CA2135253A1 (en) | 1994-11-07 | 1996-05-08 | Michael Dennis | Compound screening based on a window of chemical-messenger-independent activity |
| AU714642B2 (en) * | 1995-06-06 | 2000-01-06 | Human Genome Sciences, Inc. | G-protein receptor HTNAD29 |
| WO1997011159A1 (en) | 1995-09-20 | 1997-03-27 | Molecular Geriatrics Corporation | Yeast receptor and g-protein fusion protein |
| FR2742033B1 (fr) * | 1995-12-08 | 1998-01-16 | Achart Jacques | Appareil pour l'ouverture de coquillages de mollusques bivalves |
| US5750353A (en) | 1995-12-11 | 1998-05-12 | New England Medical Center Hospitals, Inc. | Assay for non-peptide agonists to peptide hormone receptors |
| EP0869975B1 (en) | 1995-12-11 | 2007-08-15 | New England Medical Center Hospitals, Inc. | Assay for and uses of peptide hormone receptor ligands |
| US5932779A (en) * | 1996-06-10 | 1999-08-03 | Millennium Pharmaceuticals, Inc. | Screening methods for compounds useful in the regulation of body weight |
| AU3648297A (en) | 1996-07-02 | 1998-01-21 | President And Fellows Of Harvard College | Receptor tyrosine phosphatase, and uses related thereto |
| ATE284972T1 (de) * | 1996-09-24 | 2005-01-15 | Cadus Pharmaceutical Corp | Verfahren und zusammensetzungen für die identifizierung von receptor effectoren |
| WO1998029440A1 (en) | 1996-12-27 | 1998-07-09 | Merck & Co., Inc. | Mouse galanin receptor galr2 and nucleotides encoding same |
| US6403305B1 (en) | 1997-02-06 | 2002-06-11 | Cornell Research Foundation, Inc. | Methods of identifying peptide agonists or negative antagonists of a G protein coupled receptor |
| WO1998038217A1 (en) | 1997-02-27 | 1998-09-03 | Milt Teitler | Constitutively activated serotonin receptors |
| NZ336479A (en) | 1997-04-14 | 2001-10-26 | Arena Pharm Inc | A method of identifying modulators of cell surface membrane receptors useful in the treatment of disease |
| US6555339B1 (en) * | 1997-04-14 | 2003-04-29 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated human protein-coupled receptors |
| US5891720A (en) | 1997-04-17 | 1999-04-06 | Millennium Pharmaceuticals, Inc. | Isolated DNA encoding a novel human G-protein coupled receptor |
| EP0878542A3 (en) | 1997-04-22 | 2000-04-19 | Smithkline Beecham Corporation | cDNA clone HMTMF81 that encodes a novel human 7-transmembrane receptor |
| JP2002508660A (ja) | 1997-06-12 | 2002-03-19 | スミスクライン ビーチャム コーポレーション | Ｈｍ７４ａ受容体 |
| US5955308A (en) | 1997-06-18 | 1999-09-21 | Smithkline Beecham Corporation | cDNA clone HEAOD54 that encodes a human 7-transmembrane receptor |
| US6222029B1 (en) | 1997-08-01 | 2001-04-24 | Genset | 5′ ESTs for secreted proteins expressed in brain |
| WO1999024569A1 (fr) | 1997-11-11 | 1999-05-20 | Ono Pharmaceutical Co., Ltd. | Recepteur d'acide lysophosphatidique humain et utilisation dudit recepteur |
| SE9704836D0 (sv) | 1997-12-22 | 1997-12-22 | Astra Pharma Inc | Novel receptor |
| ATE440865T1 (de) | 1998-03-26 | 2009-09-15 | Univ Leland Stanford Junior | Neue g-protein-gekoppelte rezeptoren aus säugetieren mit extrazellulären leucin-reicher region |
| JP2003514763A (ja) | 1998-04-14 | 2003-04-22 | アリーナ・フアーマシユーチカルズ・インコーポレーテツド | 非内在性の構成的に活性化されるヒトセロトニンレセプターおよびその小分子調節物質 |
| CN1231762C (zh) * | 1998-07-31 | 2005-12-14 | 阿瑞那制药公司 | 对候选化合物进行直接鉴定的方法 |
| EP1111049A4 (en) | 1998-09-03 | 2002-10-29 | Asahi Chemical Ind | New receptor protein and method for diagnosing inflammatory diseases using it |
| US20030229216A1 (en) * | 1998-10-13 | 2003-12-11 | Ruoping Chen | Constitutively activated human G protein coupled receptors |
| KR20010080882A (ko) | 1998-10-13 | 2001-08-25 | 리처드 피. 버군 쥬니어 | 구성적으로 활성화된 비내생성 인간 ｇ 단백질 결합형수용체 |
| EP1153932A1 (en) | 1999-02-19 | 2001-11-14 | Takeda Chemical Industries, Ltd. | Novel g protein-coupled receptor protein and dna thereof |
| EP1200474A1 (en) | 1999-07-15 | 2002-05-02 | Solvay Pharmaceuticals B.V. | Human g-protein coupled receptor |
| WO2001007606A1 (en) | 1999-07-27 | 2001-02-01 | Smithkline Beecham Plc | Axor21, a g-protein coupled receptor |
| JP2003510027A (ja) | 1999-08-17 | 2003-03-18 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフトング | Ｐｇｐｃｒ−３ポリペプチドおよびそのｄｎａ配列 |
| WO2001014577A1 (en) | 1999-08-24 | 2001-03-01 | Smithkline Beecham Corporation | Molecular cloning of a galanin like 7tm receptor (axor40) |
| WO2001016159A1 (en) | 1999-08-27 | 2001-03-08 | Smithkline Beecham Corporation | Gpcr, theant |
| GB9923889D0 (en) | 1999-10-08 | 1999-12-08 | Pfizer Ltd | Novel polypeptide |
| GB9924951D0 (en) | 1999-10-21 | 1999-12-22 | Pfizer Ltd | Novel polypeptide |
| EP1230361A2 (en) | 1999-10-27 | 2002-08-14 | PHARMACIA & UPJOHN COMPANY | G protein-coupled receptors expressed in human brain |
| IL149569A0 (en) | 1999-11-17 | 2002-11-10 | Arena Pharm Inc | Endogenous and non-endogenous versions of human g protein-coupled receptors |
-
1998
- 1998-10-13 US US09/170,496 patent/US6555339B1/en not_active Expired - Lifetime
-
1999
- 1999-10-12 JP JP2000576019A patent/JP4672866B2/ja not_active Expired - Fee Related
- 1999-10-12 NZ NZ510331A patent/NZ510331A/en not_active IP Right Cessation
- 1999-10-12 AU AU64307/99A patent/AU769987B2/en not_active Ceased
- 1999-10-12 DE DE1121431T patent/DE1121431T1/de active Pending
- 1999-10-12 IL IL14196599A patent/IL141965A0/xx active IP Right Grant
- 1999-10-12 WO PCT/US1999/023935 patent/WO2000021987A2/en not_active Ceased
- 1999-10-12 KR KR1020017004587A patent/KR100598752B1/ko not_active Expired - Fee Related
- 1999-10-12 JP JP2000575892A patent/JP4685241B2/ja not_active Expired - Fee Related
- 1999-10-12 AT AT99951991T patent/ATE318311T1/de not_active IP Right Cessation
- 1999-10-12 CA CA002342314A patent/CA2342314A1/en not_active Abandoned
- 1999-10-12 CN CNB99812091XA patent/CN1329511C/zh not_active Expired - Fee Related
- 1999-10-12 ES ES99951991T patent/ES2163384T3/es not_active Expired - Lifetime
- 1999-10-12 EP EP99951991A patent/EP1121431B9/en not_active Expired - Lifetime
- 1999-10-12 DK DK99951991T patent/DK1121431T5/da active
- 1999-10-12 DE DE69929993T patent/DE69929993T4/de not_active Expired - Lifetime
- 1999-10-12 DE DE69929993A patent/DE69929993D1/de not_active Expired - Lifetime
- 1999-10-12 WO PCT/US1999/023938 patent/WO2000022129A1/en not_active Ceased
-
2001
- 2001-03-12 IL IL141965A patent/IL141965A/en not_active IP Right Cessation
-
2002
- 2002-09-20 US US10/251,385 patent/US7410777B2/en not_active Expired - Fee Related
-
2004
- 2004-07-08 AU AU2004203102A patent/AU2004203102B2/en not_active Ceased
-
2008
- 2008-01-16 AU AU2008200231A patent/AU2008200231A1/en not_active Abandoned
-
2011
- 2011-01-04 AU AU2011200016A patent/AU2011200016A1/en not_active Abandoned
- 2011-02-07 AU AU2011200511A patent/AU2011200511A1/en not_active Abandoned
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2163384T3 (es) | Receptores acoplados a proteinas g humanos, activados de forma constitutiva, no endogenos. | |
| ES2308759T3 (es) | Receptores acoplados a proteina g humanos huerfanos. | |
| KR20010080882A (ko) | 구성적으로 활성화된 비내생성 인간 ｇ 단백질 결합형수용체 | |
| AU1769601A (en) | Endogenous and non-endogenous versions of human G protein-coupled receptors | |
| ES2264267T3 (es) | Nuevas proteinas de receptores copulados a proteina g. | |
| ES2278755T3 (es) | Regulacion del receptor acoplado a proteinas g de tipo dopamina humano. | |
| US20130165633A1 (en) | Endogenous and Non-Endogenous Versions of Human G Protein-Coupled Receptors | |
| US20060240523A1 (en) | Endogenous and non-endogenous versions of human G protein-coupled receptors | |
| US20130309766A1 (en) | Endogenous and Non-Endogenous Versions of Human G Protein-Coupled Receptors | |
| CA2429860A1 (en) | Endogenous and non-endogenous versions of human g protein-coupled receptors | |
| ES2282304T3 (es) | Procedimiento para seleccionar antiplaquetas. | |
| ES2305229T3 (es) | Receptor acoplado a la proteina g humana. | |
| US7119190B2 (en) | Endogenous and non-endogenous versions of human G protein-coupled receptors | |
| ES2241842T3 (es) | Regulacion del receptor acoplado a proteinas g tipo receptor adrenergico alfa 1(a) humano. | |
| US8440391B2 (en) | Constitutively activated human G protein coupled receptors | |
| ES2271020T3 (es) | Uso del receptor acoplado a proteina g de tipo latrofilina en humanos en procedimientos de monitorizacion. | |
| US20070072248A1 (en) | Constitutively activated human G protein coupled receptors | |
| JP4768946B2 (ja) | ヒトｇタンパク質共役型受容体の内因性および非内因性型 | |
| AU2004202476A1 (en) | Human G Protein-Coupled Receptors | |
| EP1676861A2 (en) | Non-endogenous, constitutively activated human G protein-coupled receptors | |
| US20150153327A1 (en) | Endogenous and Non-Endogenous Versions of Human G Protein-Coupled Receptors | |
| HK1038040B (en) | Non-endogenous, constitutively activated human g protein-coupled receptors | |
| JP2003525018A6 (ja) | 非内在性の構成的に活性化されるヒトｇタンパク質共役型受容体 | |
| McLean | Ligand regulation of β1-and β2-adrenergic receptors and their GFP-tagged forms | |
| HK1091214A (en) | Non-endogenous, constitutively activated human g protein-coupled receptors |